Digex NF

Pronunciation: HYE-oh-SYE-a-meen/FEN-il-tole-OX-a-meen
Generic Name: Hyoscyamine/Phenyltoloxamine
Brand Name: Digex NF

Digex NF is used for:

Relieving symptoms of indigestion (eg, feeling of fullness, gas, bloating). It is also used to treat certain stomach and intestinal conditions, including spasms and cramps. It may also be used for other conditions as determined by your doctor.

Digex NF is an anticholinergic and antihistamine combination. It works by decreasing the motion of muscles in the stomach, intestines, and bladder. It also decreases the production of stomach acid.

Do NOT use Digex NF if:

• you are allergic to any ingredient in Digex NF


• you have severe esophagus problems (eg, irritation, narrowing); a blockage of the stomach, bowel, or bladder; bowel motility problems; or severe bowel problems (eg, severe ulcerative colitis, toxic megacolon)


• you have glaucoma, myasthenia gravis, or heart problems caused by severe bleeding


• you are taking sodium oxybate (GHB)


• you are taking potassium chloride capsules or tablets

Contact your doctor or health care provider right away if any of these apply to you.

Before using Digex NF:

Some medical conditions may interact with Digex NF. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have lung or breathing problems (eg, asthma), nerve problems, prostate problems, esophagus problems (eg, reflux), stomach or bowel problems, heart or blood vessel problems (eg, fast or irregular heartbeat, heart failure, coronary heart disease), hiatal hernia, kidney problems, an overactive thyroid, high blood pressure, urinary problems, paralysis, or brain damage, or if you are at risk for glaucoma


• if you have diarrhea or fever, have trouble urinating, have been very ill, or are in poor health

Some MEDICINES MAY INTERACT with Digex NF. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Potassium tablets or capsules because they may not be able to move through the stomach and bowel as well when taken with Digex NF; this may increase the risk of their side effects


• Narcotic pain medicines (eg, codeine) because the risk of their side effects may be increased by Digex NF


• Amantadine, antihistamines (eg, diphenhydramine), haloperidol, monoamine oxidase inhibitors (MAOIs) (eg, phenelzine), other anticholinergics (eg, scopolamine), phenothiazines (eg, thioridazine), sodium oxybate (GHB), or tricyclic antidepressants (eg, amitriptyline) because they may increase the risk of Digex NF's side effects


• Ketoconazole or metoclopramide because their effectiveness may be decreased by Digex NF

This may not be a complete list of all interactions that may occur. Ask your health care provider if Digex NF may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Digex NF:

Use Digex NF as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Digex NF by mouth with food as directed by your doctor.


• If you also take antacids, take Digex NF before meals and the antacid after meals, unless directed otherwise by your doctor.


• If you open the capsule, do not breathe in the powder. Some patients may experience an allergic reaction (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue) from breathing in the powder.


• If you miss a dose of Digex NF, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Digex NF.

Important safety information:

• Digex NF may cause drowsiness, dizziness, or blurred vision. These effects may be worse if you take it with alcohol or certain medicines. Use Digex NF with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Do not drink alcohol or use medicines that may cause drowsiness (eg, sleep aids, muscle relaxers) while you are using Digex NF; it may add to their effects. Ask your pharmacist if you have questions about which medicines may cause drowsiness.


• Do NOT take more than the recommended dose or use for longer than prescribed without checking with your doctor.


• Do not become overheated or dehydrated in hot weather or while you are being active; heatstroke may occur.


• Drink plenty of fluids, maintain good oral hygiene, and suck on sugarless hard candy to relieve dry mouth.


• Proper dental care is important while you are taking Digex NF. Brush and floss your teeth and visit the dentist regularly.


• Digex NF may make your eyes more sensitive to sunlight. It may help to wear sunglasses.


• Tell your doctor or dentist that you take Digex NF before you receive any medical or dental care, emergency care, or surgery.


• Use Digex NF with caution in the ELDERLY; they may be more sensitive to its effects, especially constipation, trouble urinating, dry mouth, drowsiness, agitation, confusion, excitability, or memory problems.


• Caution is advised when using Digex NF in CHILDREN; they may be more sensitive to its effects, including excitability.


• PREGNANCY and BREAST-FEEDING: It is not known if Digex NF can cause harm to the fetus. If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Digex NF while you are pregnant. Digex NF is found in breast milk. If you are or will be breast-feeding while taking Digex NF, check with your doctor. Discuss any possible risks to your baby.

Possible side effects of Digex NF:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Bloated feeling; blurred vision; constipation; decreased sweating; dizziness; drowsiness; dry mouth; enlarged pupils; excitability; headache; nausea; nervousness; trouble sleeping; weakness.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); agitation; behavior changes; confusion; decreased sexual ability; diarrhea; difficulty focusing eyes; disorientation; exaggerated sense of well-being; fast or irregular heartbeat; fever; hallucinations; loss of consciousness; loss of coordination; memory loss; mental or mood changes; severe or persistent trouble sleeping; speech changes; taste changes or loss; trouble urinating; unusual tiredness or weakness; vision changes; vomiting.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

See also: Digex NF side effects (in more detail)

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include disorientation; excessive thirst or excitability; fever; hot, dry skin; seizures; severe dry mouth; severe or persistent blurred vision, dizziness, headache, nausea, or vomiting; trouble breathing or swallowing.

Proper storage of Digex NF:

Store Digex NF at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Digex NF out of the reach of children and away from pets.

General information:

• If you have any questions about Digex NF, please talk with your doctor, pharmacist, or other health care provider.


• Digex NF is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Digex NF. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Digex NF resources

• Digex NF Side Effects (in more detail)
• Digex NF Use in Pregnancy & Breastfeeding
• Digex NF Drug Interactions
• Digex NF Support Group
• 0 Reviews · Be the first to review/rate this drug

Dicloxacillin Sodium

Class: Penicillinase-resistant Penicillins
Chemical Name: [2S - (2α,5α,6β)] - 6 - [[[3 - (2,6 - Dichlorophenyl) - 5 - methyl - 4 - isoxazolyl]carbonyl]amino] - 3,3 - dimethyl - 7 - oxo - 4 - thia - 1 - azabicyclo[3.2.0]heptane - 2 - carboxylic acid monosodium salt monohydrate
CAS Number: 13412-64-1

Introduction

Antibacterial; β-lactam antibiotic; isoxazolyl penicillin classified as a penicillinase-resistant penicillin.^{1 2 6 7 18 29 30 37}

Uses for Dicloxacillin Sodium

Staphylococcal Infections

Treatment of infections caused by, or suspected of being caused by, susceptible penicillinase-resistant staphylococci.^{1 2 3 4 5 6 7 8}

Should not be used for initial treatment of severe, life-threatening infections, including endocarditis, but may be used as follow-up after a parenteral penicillinase-resistant penicillin (nafcillin, oxacillin).^{1 2 5 6 8 9}

If used empirically, consider whether staphylococci resistant to penicillinase-resistant penicillins (oxacillin-resistant [methicillin-resistant] staphylococci) are prevalent in the hospital or community.^a (See Staphylococci Resistant to Penicillinase-resistant Penicillins under Cautions.)

Dicloxacillin Sodium Dosage and Administration

Administration

Oral Administration

Administer orally at least 1 hour before or 2 hours after meals.^{1 2}

Should not be used for initial treatment of severe infections and should not be relied on in patients with nausea, vomiting, gastric dilatation, cardiospasm, or intestinal hypermotility.^{1 2 6 9}

Dosage

Available as dicloxacillin sodium; dosage expressed in terms of dicloxacillin.^{1 2}

Duration of treatment depends on type and severity of infection and should be determined by the clinical and bacteriologic response of the patient.^{1 2 5 6 8} Usually continued for ≥48 hours after cultures are negative and patient becomes afebrile and asymptomatic.^{1 2} For severe staphylococcal infections, continue therapy for ≥14 days;^{1 2 5 6} more prolonged therapy is necessary for treatment of osteomyelitis, endocarditis, or other metastatic infections.^{1 2 5 6 13 54}

Pediatric Patients

Staphylococcal Infections

Mild to Moderate Infections

Oral

Children weighing <40 kg: 12.5 mg/kg daily given in divided doses every 6 hours.^{1 2 6 11}

Children weighing ≥40 kg: 125 mg every 6 hours.^{1 2 6}

Children ≥1 month of age: AAP recommends 25–50 mg/kg daily in 4 divided doses.⁹

More Severe Infections

Oral

Children weighing <40 kg: 25 mg/kg daily given in divided doses every 6 hours;^{1 2} higher dosage may be necessary depending on severity of infection.^{6 11}

Children weighing ≥40 kg: 250 mg every 6 hours;^{1 2} higher dosage may be necessary depending on severity of infection.⁶

Inappropriate for severe infections per AAP.⁹

Acute or Chronic Osteomyelitis

Oral

50–100 mg/kg daily given in divided doses every 6 hours as follow-up to initial parenteral therapy.^{12 13 14 16 54} If an oral regimen is used, compliance must be assured and some clinicians suggest that serum bactericidal titers (SBTs) be used to monitor adequacy of therapy and adjust dosage.^{13 14 15 16 17 53 54}

When used as follow-up in treatment of acute osteomyelitis, oral regimen usually given for 3–6 weeks or until total duration of parenteral and oral therapy is ≥6 weeks;^{12 13 14 16 54} when used as follow-up in treatment of chronic osteomyelitis, oral regimen usually given for ≥1–2 months and has been given for as long as 1–2 years.^{13 18 54}

Adults

Staphylococcal Infections

Mild to Moderate Infections

Oral

125 mg every 6 hours.^{1 2 6}

More Severe Infections

Oral

250 mg every 6 hours;^{1 2} higher dosage may be necessary depending on severity of infection.⁶

Special Populations

Renal Impairment

Dosage adjustment generally unnecessary in patients with renal impairment.^{19 20 21}

Cautions for Dicloxacillin Sodium

Contraindications

• 
  

  Known hypersensitivity to any penicillin.^{1 2 6}

  
  

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity Reactions

Serious and occasionally fatal hypersensitivity reactions, including anaphylaxis, reported with penicillins.^{1 2} Anaphylaxis occurs most frequently with parenteral penicillins but has occurred with oral penicillins.^{1 2}

Prior to initiation of therapy, make careful inquiry regarding previous hypersensitivity reactions to penicillins, cephalosporins, or other drugs.^{1 2} Partial cross-allergenicity occurs among penicillins and other β-lactam antibiotics including cephalosporins and cephamycins.^{1 2 22 23 24 25}

If a severe hypersensitivity reaction occurs, discontinue immediately and institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, maintenance of an adequate airway and oxygen).^{1 2}

General Precautions

Superinfection

Possible emergence and overgrowth of nonsusceptible bacteria or fungi.^{1 2} Discontinue and institute appropriate therapy if superinfection occurs.^{1 2}

Laboratory Monitoring

Periodically assess organ system functions, including renal, hepatic, and hematopoietic, during prolonged therapy.¹

Peform urinalysis and determine serum creatinine and BUN concentrations prior to and periodically during therapy.^{1 2}

To monitor for hepatotoxicity, determine AST and ALT concentrations prior to and periodically during therapy.^{1 2}

Because adverse hematologic effects have occurred with penicillinase-resistant penicillins, total and differential WBC counts should be performed prior to and 1–3 times weekly during therapy.^{1 2 5 6 26 27}

Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of dicloxacillin and other antibacterials, use only for treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria.

When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing.^{1 2} In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.^{1 2}

Staphylococci Resistant to Penicillinase-resistant Penicillins

Consider that staphylococci resistant to penicillinase-resistant penicillins (referred to as oxacillin-resistant [methicillin-resistant] staphylococci) are being reported with increasing frequency.^a

If dicloxacillin used empirically for treatment of any infection suspected of being caused by staphylococci, the drug should be discontinued and appropriate anti-infective therapy substituted if the infection is found to be caused by any organism other than penicillinase-producing staphylococci susceptible to penicillinase-resistant penicillins.^{1 2} If staphylococci resistant to penicillinase-resistant penicillins (oxacillin-resistant staphylococci) are prevalent in the hospital or community, empiric therapy of suspected staphylococcal infections should include another appropriate anti-infective (e.g., vancomycin).^a

Sodium Content

Each 250-mg capsule contains approximately 0.6 mEq of sodium.⁵²

Specific Populations

Pregnancy

Category B.^{1 2 6}

Lactation

Distributed into milk.^{1 2 6 28} Use with caution.^{1 2 6}

Pediatric Use

Elimination of penicillins is delayed in neonates because of immature mechanisms for renal excretion; abnormally high serum concentrations may occur in this age group.^{1 2 6}

If used in neonates, monitor closely for clinical and laboratory evidence of toxic or adverse effects, determine serum concentrations frequently, and make appropriate reductions in dosage and frequency of administration when indicated.^{1 2 6}

Common Adverse Effects

GI effects (nausea, vomiting, epigastric distress, loose stools, diarrhea, flatulence); hypersensitivity reactions.^a

Interactions for Dicloxacillin Sodium

Specific Drugs

Drug	Interaction	Comments
Aminoglycosides	In vitro evidence of synergistic antibacterial effects against penicillinase-producing and nonpenicillinase-producing S. aureusa
Anticoagulants, oral (warfarin)	Possible decreased hypothrombinemic effecta	Monitor PTs and adjust anticoagulant dosage if indicateda
Probenecid	Decreased renal tubular secretion and increased and prolonged dicloxacillin plasma concentrations.1 2 a
Tetracyclines	Possible antagonism1 2 a	Concomitant use not recommended1 2 a

Dicloxacillin Sodium Pharmacokinetics

Absorption

Bioavailability

Rapidly, but incompletely, absorbed from GI tract.^{1 2 7 33}

35–76% of an oral dose absorbed from GI tract;^{33 34 35} peak serum concentrations generally attained within 0.5–2 hours.^{1 2 35 36}

Food

Food in the GI tract generally decreases the rate and extent of absorption.^{1 2 4 6 7 29 35}

Distribution

Extent

Distributed into bone,^{4 39} bile,^{1 2} pleural fluid,^{1 2 4 7} ascitic fluid,⁴ and synovial fluid.^{4 40}

Only minimal concentrations attained in CSF.²

Crosses the placenta⁴² and is distributed into milk.^{1 2 6 28}

Plasma Protein Binding

95–99% bound to serum proteins.^{1 2 7 31 34 37 41}

Elimination

Metabolism

Partially metabolized to active and inactive metabolites.^{4 43 46 47}

Approximately 10% of absorbed drug is hydrolyzed to penicilloic acids which are microbiologically inactive;⁴⁶ also hydroxylated to a small extent to a microbiologically active metabolite which appears to be slightly less active than dicloxacillin.⁴⁷

Elimination Route

Dicloxacillin and its metabolites rapidly eliminated in urine mainly by tubular secretion and glomerular filtration.^{1 2 7 29 43 47} Also partly excreted in feces via biliary elimination.⁴

31–65% of a dose excreted in urine as unchanged drug and active metabolites within 6–8 hours;^{4 31 32 34 36 46 47} approximately 10–20% of this is the active metabolite.^{4 47}

Only minimally removed by hemodialysis^{4 10 20 34 43 44 49} or peritoneal dialysis.^{4 44 49}

Half-life

Adults with normal renal function: 0.6–0.8 hours.^{1 2 4 33 34 43 44 45}

Children 2–16 years of age: average half-life is 1.9 hours.³⁹

Neonates: half-life is longer than in older children.^{4 6}

Special Populations

Patients with renal impairment: serum half-life is slightly prolonged and may range from 1–2.2 hours in those with severe renal impairment.^{4 33 34 45}

Patients with cystic fibrosis eliminate dicloxacillin approximately 3 times faster than healthy individuals.^{7 48}

Stability

Storage

Oral

Capsules

15–30°C⁵² in tight containers.⁵⁰

Actions and SpectrumActions

• 
  

  Based on spectrum of activity, classified as a penicillinase-resistant penicillin.^{1 2 6 7 29 30 31 32}

  
  


• 
  

  Usually bactericidal.^{1 2}

  
  


• 
  

  Like other β-lactam antibiotics, antibacterial activity results from inhibition of bacterial cell wall synthesis.^{1 2}

  
  


• 
  

  Spectrum of activity includes many gram-positive aerobic cocci, some gram-positive bacilli, and a few gram-negative aerobic cocci; generally inactive against gram-negative bacilli and anaerobic bacteria.^a Inactive against mycobacteria, Mycoplasma, Rickettsia, fungi, and viruses.^a

  
  


• 
  

  Gram-positive aerobes: active in vitro against penicillinase-producing and nonpenicillinase-producing Staphylococcus aureus and S. epidermidis, S. pyogenes (group A β-hemolytic streptococci), S. agalactiae (group B streptococci), groups C and G streptococci, S. pneumoniae, and some viridans streptococci.^a Enterococci (including E. faecalis) usually are resistant.^a

  
  


• 
  

  Like other penicillinase-resistant penicillins, dicloxacillin is resistant to inactivation by staphylococcal penicillinases and is active against many penicillinase-producing strains of S. aureus and S. epidermidis resistant to natural penicillins, aminopenicillins, or extended-spectrum penicillins.^{1 2 4 6 7 30 31 32}

  
  


• 
  

  Staphylococci resistant to penicillinase-resistant penicillins (referred to as oxacillin-resistant [methicillin-resistant] staphylococci) are being reported with increasing frequency.^a Complete cross-resistance occurs among the penicillinase-resistant penicillins (dicloxacillin, nafcillin, oxacillin).^a

  
  

Advice to Patients

• 
  

  Advise patients that antibacterials (including dicloxacillin) should only be used to treat bacterial infections and not used to treat viral infections (e.g., the common cold).

  
  


• 
  

  Importance of completing full course of therapy, even if feeling better after a few days.^{1 2}

  
  


• 
  

  Advise patients that skipping doses or not completing the full course of therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with dicloxacillin or other antibacterials in the future.

  
  


• 
  

  Importance of taking dicloxacillin 1 hour before or 2 hours after meals.^{1 2}

  
  


• 
  

  Importance of discontinuing dicloxacillin and notifying clinician if they develop shortness of breath, wheezing, rash, mouth irritation, black tongue, sore throat, nausea, vomiting, diarrhea, fever, swollen joints, or any unusual bleeding or bruising during dicloxacillin treatment.^{1 2}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.^{1 2}

  
  


• 
  

  Importance of women informing clinician if they are or plan to become pregnant or to breast-feed.¹

  
  


• 
  

  Importance of informing patients of other important precautionary information. (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Dicloxacillin Sodium

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules	250 mg (of dicloxacillin)*	Dicloxacillin Sodium	Sandoz, Teva
		500 mg (of dicloxacillin)*	Dicloxacillin Sodium	Sandoz, Teva

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Dicloxacillin Sodium 250MG Capsules (SANDOZ): 30/$18.99 or 90/$35.97

Dicloxacillin Sodium 500MG Capsules (SANDOZ): 30/$24.99 or 90/$53.97

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions May 2004. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

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2. Teva Pharmaceuticals. Dicloxacillin sodium capsules, USP prescribing information. Sellersville, PA; 1997 Jul.

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4. Neu HC. Antistaphylococcal penicillins. Med Clin North Am. 1982; 66:51-60. [PubMed 7038340]

5. Kunin CM. Penicillinase-resistant penicillins. JAMA. 1977; 237:1605-6. [PubMed 576661]

6. US Food and Drug Administration. Penicillinase-resistant penicillin human prescription drugs class labeling guideline for professional labeling. [Notice of availability published in: Fed Regist. 1982; 47:41636.] Available from: Professional Labeling Branch, Division of Drug Advertising and Labeling, Food and Drug Administration, Rockville, MD.

7. Kucers A, Crowe S, Grayson ML et al, eds. The use of antibiotics. A clinical review of antibacterial, antifungal, and antiviral drugs. 5th ed. Jordan Hill, Oxford: Butterworth-Heinemann; 1997: 3-226.

8. Behrman RE, Kliegman RM, Jenson HB, eds. Nelson textbook of pediatrics. 16th ed. Philadelphia: WB Saunders Company; 2000.

9. Committee on Infectious Diseases, American Academy of Pediatrics. 2000 Red book: report of the Committee on Infectious Diseases. 25th ed. Elk Grove Village, IL: American Academy of Pediatrics; 1997:514-26,660.

10. Deresinski SC, Stevens DA. Clinical evaluation of parenteral dicloxacillin. Curr Ther Res Clin Exp. 1975; 18:151-63. [PubMed 809231]

11. Gunn VL, Nechyba C, eds. The Harriet Lane handbook: a manual for pediatric house officers. 16th ed. Philadelphia, PA: Mosby: 2002:660-1.

12. Bryson YJ, Connor JD, LeClerc M et al. High-dose dicloxacillin treatment of acute staphylococcal osteomyelitis in children. J Pediatr. 1979; 94:673-5. [PubMed 430319]

13. Dunkle LM, Brock N. Long-term follow-up of ambulatory management of osteomyelitis. Clin Pediatr. 1982; 21:650-5.

14. Kaplan SL, Mason EO, Feigin RD. Clindamycin versus nafcillin or methicillin in the treatment of Staphylococcus aureus osteomyelitis in children. South Med J. 1982; 75:138-42. [IDIS 145829] [PubMed 7036354]

15. Waldvogel FA, Vasey H. Osteomyelitis: the past decade. N Engl J Med. 1980; 303:360-70. [IDIS 119618] [PubMed 6993944]

16. Prober CG, Yeager AS. Use of the serum bactericidal titer to assess the adequacy of oral antibiotic therapy in the treatment of acute hematogenous osteomyelitis. J Pediatr. 1979; 95:131-5. [PubMed 113517]

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19. Cheigh JS. Drug administration in renal failure. Am J Med. 1977; 62:555-63. [PubMed 851131]

20. Bennett WM, Aronoff GR, Morrison G et al. Drug prescribing in renal failure: dosing guidelines for adults. Am J Kidney Dis. 1983; 3:155-93. [PubMed 6356890]

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23. Erffmeyer JE. Adverse reactions to penicillin. Ann Allergy. 1981; 47:288-300. [PubMed 6171185]

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25. Sullivan TJ, Wedner HJ, Shatz GS et al. Skin testing to detect penicillin allergy. J Allergy Clin Immunol. 1981; 68:171-80. [IDIS 140792] [PubMed 6267115]

26. Carpenter J. Neutropenia induced by semisynthetic penicillin. South Med J. 1980; 73:745-7. [IDIS 128169] [PubMed 7394597]

27. Homayouni H, Gross PA, Setia U et al. Leukopenia due to penicillin and cephalosporin homologues. Arch Intern Med. 1979; 139:827-8. [PubMed 454076]

28. Matsuda S. Transfer of antibiotics into maternal milk. Biol Res Pregnancy. 1984; 5:57-60.

29. Marcy SM, Klein JO. The isoxazolyl penicillins: oxacillin, cloxacillin, and dicloxacillin. Med Clin North Am. 1970; 52:1127-43.

30. Selwyn S. The mechanisms and range of activity of penicillins and cephalosporins. In: Selwyn S, ed. The beta-lactam antibiotics: penicillins and cephalosporins in perspective. London: Hodder and Stoughton; 1980:56-90.

31. Gravenkemper CF, Bennett JV, Brodie JL et al. Dicloxacillin: in vitro and pharmacologic comparisons with oxacillin and cloxacillin. Arch Intern Med. 1965; 116:340-5. [PubMed 14325906]

32. Hammerstrom CF, Cox F, McHenry MC et al. Clinical, laboratory, and pharmacological studies of dicloxacillin. Antimicrob Agents Chemother. 1966:69-74.

33. Nauta EH, Mattie H. Dicloxacillin and cloxacillin: pharmacokinetics in healthy and hemodialysis subjects. Clin Pharmacol Ther. 1976; 20:98-108. [PubMed 1277730]

34. Barza M, Weinstein L. Pharmacokinetics of the penicillins in man. Clin Pharmacokinet. 1976; 1:297-308. [PubMed 797501]

35. Doluisio JT, LaPiana JC, Wilkinson GR et al. Pharmacokinetic interpretation of dicloxacillin levels in serum after extravascular administration. Antimicrob Agents Chemother. 1969:49-55.

36. DeFelice EA. Serum levels, urinary recovery, and safety of dicloxacillin, a new semisynthetic penicillin, in normal volunteers. J Clin Pharmacol. 1967; (Sep-Oct):275-7.

37. Hou JP, Poole JW. β-Lactam antibiotics: their physiochemical properties and biological activities in relation to structure. J Pharm Sci. 1971; 60:503-27. [PubMed 4336386]

38. Bass JW, Bruhn FW, Merritt WT et al. Comparison of oral penicillinase-resistant penicillins: contrasts between agents and assays. South Med J. 1982; 75:408-10. [IDIS 150080] [PubMed 7041278]

39. Tetzlaff TR, Howard JB, McCracken GH et al. Antibiotic concentrations in pus and bone in children with osteomyelitis. J Pediatr. 1978; 92:135-40. [IDIS 172809] [PubMed 619056]

40. Nelson JD, Howard JB, Shelton S. Oral antibiotic therapy for skeletal infections of children. J Pediatr. 1978; 92:131-4. [IDIS 172808] [PubMed 619055]

41. Kunin CM. Clinical significance of protein binding of the penicillins. Ann NY Acad Sci. 1967; 145:282-90. [PubMed 4998178]

42. Depp R, Kind AC, Kirby WM et al. Transplacental passage of methicillin and dicloxacillin into the fetus and amniotic fluid. Am J Obstet Gynecol. 1970; 107:1054-7. [PubMed 5429971]

43. Bergan T. Penicillins. In: Schonfeld H, ed. Antibiotics and chemotherapy. Vol 25. Basel: S. Karger; 1978:1-122.

44. Giusti DL. A review of the clinical use of antimicrobial agents in patients with renal and hepatic insufficiency: the penicillins. Drug Intell Clin Pharm. 1973; 7:62-74.

45. Rosenblatt JE, Kind AC, Brodie JL et al. Mechanisms responsible for the blood level differences of isoxazolyl penicillins: oxacillin, cloxacillin, and dicloxacillin. Arch Intern Med. 1968; 121:345-8. [PubMed 5645708]

46. Cole M, Kening MD, Hewitt VA. Metabolism of penicillins to penicilloic acids and 6-aminopenicillanic acid in man and its significance in assessing penicillin absorption. Antimicrob Agents Chemother. 1973; 3:463-8. [PubMed 4364176]

47. Thijssen HH, Mattie H. Active metabolites of isoxazolylpenicillins in humans. Antimicrob Agents Chemother. 1976; 10:441-6. [PubMed 825029]

48. Jusko WJ, Mosovich LL, Gerbracht LM et al. Enhanced renal excretion of dicloxacillin in patients with cystic fibrosis. Pediatrics. 1975; 56:1038-44. [PubMed 1196754]

49. Neu HC. Penicillins: microbiology, pharmacology, and clinical use. In: Kagan BM, ed. Antimicrobial therapy. 3rd ed. Philadelphia: WB Saunders Company; 1980:20-34.

50. The United States pharmacopeia, 26th rev, and The national formulary, 21st ed. Rockville, MD: The United States Pharmacopeial Convention, Inc; 2003:597-8,1261-3,1355-7,2571-2.

51. Newton DW, Kluza RB. pK_a Values of medicinal compounds in pharmacy practice. Drug Intell Clin Pharm. 1978; 12:546-54.

52. Porter EG (Bristol Laboratories, Syracuse, NY): Personal communication; 1984 Dec 28.

53. Hedstrom SA. Treatment of chronic staphylococcal osteomyelitis with cloxacillin and dicloxacillin—a comparative study in 12 patients. Scand J Infect Dis. 1975; 7:55-7. [PubMed 1145134]

54. Armstrong EP, Rush DR. Treatment of osteomyelitis. Clin Pharm. 1983; 2:213-24. [IDIS 170639] [PubMed 6349907]

a. AHFS Drug Information 2004. McEvoy GK, ed. Penicillinase-resistant Penicillins General Statement. American Society of Health-System Pharmacists; 2004:328-34.

More Dicloxacillin Sodium resources

• Dicloxacillin Sodium Side Effects (in more detail)
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• Dicloxacillin Sodium Drug Interactions
• Dicloxacillin Sodium Support Group
• 0 Reviews for Dicloxacillin Sodium - Add your own review/rating

• dicloxacillin Concise Consumer Information (Cerner Multum)


• Dicloxacillin MedFacts Consumer Leaflet (Wolters Kluwer)


• Dicloxacillin Prescribing Information (FDA)


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• Pharyngitis
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Dacogen

Generic Name: decitabine (de SIT a been)

Brand Names: Dacogen

What is decitabine?

Decitabine is a cancer medication that interferes with the growth and spread of cancer cells in the body.

Decitabine is used to treat myelodysplastic syndromes (certain types of blood or bone marrow cancer).

Decitabine may also be used for purposes not listed in this medication guide.

What is the most important information I should know about decitabine?

Before receiving this medication, tell your doctor if you have liver or kidney disease.

Do not use decitabine if you are pregnant. It could harm the unborn baby. Use effective birth control, and tell your doctor if you become pregnant during treatment. If a man fathers a child while using this medication, the baby may have birth defects. Use a condom to prevent pregnancy during your treatment. Continue using condoms for at least 2 months after you stop receiving decitabine. You should not breast-feed while you are receiving decitabine.

Decitabine can lower blood cells that help your body fight infections. Avoid being near people who are sick or have infections. Avoid activities that may increase your risk of bleeding or injury. Your blood may need to be tested often. Visit your doctor regularly.

What should I discuss with my health care provider before receiving decitabine?

To make sure you can safely take decitabine, tell your doctor if you have any of these other conditions:

• 
  

  kidney disease; or

  
  


• 
  

  liver disease.

  
  

FDA pregnancy category D. Do not use decitabine if you are pregnant. It could harm the unborn baby. Use effective birth control, and tell your doctor if you become pregnant during treatment. If a man fathers a child while using this medication, the baby may have birth defects. Use a condom to prevent pregnancy during your treatment. Continue using condoms for at least 2 months after you stop receiving decitabine. It is not known whether decitabine passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are receiving decitabine.

How is decitabine given?

Decitabine is injected into a vein through an IV. You will receive this injection in a clinic or hospital setting. Decitabine must be given slowly, and the IV infusion can take up to 3 hours to complete.

In most cases, a decitabine injection is given every 8 hours for 3 days. This 3-day treatment is usually repeated every 6 weeks. You will most likely receive at least 4 of these treatments.

You may be given other medications to prevent nausea or vomiting while you are receiving decitabine.

Decitabine can lower blood cells that help your body fight infections. This can make it easier for you to bleed from an injury or get sick from being around others who are ill. Your blood may need to be tested often. Your kidney or liver function may also need to be tested. Visit your doctor regularly.

What happens if I miss a dose?

Call your doctor for instructions if you miss an appointment for your decitabine injection.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include some of the serious side effects listed in this medication guide.

What should I avoid while receiving decitabine?

Avoid being near people who are sick or have infections. Tell your doctor at once if you develop signs of infection.

Avoid activities that may increase your risk of bleeding or injury. Use extra care to prevent bleeding while shaving or brushing your teeth.

Decitabine side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have a serious side effect such as:

• 
  

  fever, chills, body aches, cough, sore throat, flu symptoms;

  
  


• 
  

  easy bruising, unusual bleeding (nose, mouth, vagina, or rectum), purple or red pinpoint spots under your skin;

  
  


• 
  

  pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating;

  
  


• 
  

  white patches or sores inside your mouth or on your lips; or

  
  


• 
  

  stabbing chest pain, wheezing, feeling short of breath, cough with yellow or green mucus;

  
  


• 
  

  swelling, pain, tenderness, or redness anywhere on your body; or

  
  


• 
  

  electrolyte imbalance (confusion, uneven heart rate, extreme thirst, increased urination, jerking muscle movements, leg discomfort, muscle weakness or limp feeling).

  
  

Less serious side effects may include:

• 
  

  headache, dizziness;

  
  


• 
  

  tired feeling;

  
  


• 
  

  nausea, vomiting, stomach pain, diarrhea, constipation;

  
  


• 
  

  cough;

  
  


• 
  

  increased thirst, increased urination, hunger, dry mouth, drowsiness;

  
  


• 
  

  joint pain; or

  
  


• 
  

  sleep problems (insomnia).

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect decitabine?

There may be other drugs that can interact with decitabine. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

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• Decitabine Professional Patient Advice (Wolters Kluwer)

Compare Dacogen with other medications

• Myelodysplastic Syndrome

Where can I get more information?

• Your doctor or pharmacist can provide more information about decitabine.

See also: Dacogen side effects (in more detail)

Deferoxamine

Dosage Form: injection, powder, lyophilized, for solution
Deferoxamine Mesylate for Injection USP

Rx ONLY

Deferoxamine Description

Deferoxamine Mesylate for Injection USP is an iron-chelating agent, available in vials for intramuscular, subcutaneous, and intravenous administration. Deferoxamine mesylate for injection is supplied as vials containing 500 mg and 2 g of Deferoxamine mesylate USP in sterile, lyophilized form. Deferoxamine mesylate is N-[5-[3-[(5-aminopentyl)hydroxycarbamoyl]propionamido]pentyl]-3-[[5-(N-hydroxyacetamido) pentyl]carbamoyl]propionohydroxamic acid monomethanesulfonate (salt), and its structural formula is:

Molecular Formula: C25H48N6O8•CH4O3S

Molecular Weight = 656.79

Deferoxamine mesylate USP is a white to off-white powder. It is freely soluble in water and slightly soluble in methanol.

Deferoxamine - Clinical Pharmacology

Deferoxamine mesylate chelates iron by forming a stable complex that prevents the iron from entering into further chemical reactions. It readily chelates iron from ferritin and hemosiderin but not readily from transferrin; it does not combine with the iron from cytochromes and hemoglobin. Deferoxamine mesylate does not cause any demonstrable increase in the excretion of electrolytes or trace metals. Theoretically, 100 parts by weight of Deferoxamine mesylate is capable of binding approximately 8.5 parts by weight of ferric iron.

Deferoxamine mesylate is metabolized principally by plasma enzymes, but the pathways have not yet been defined. The chelate is readily soluble in water and passes easily through the kidney, giving the urine a characteristic reddish color. Some is also excreted in the feces via the bile.

Indications and Usage for Deferoxamine

Deferoxamine mesylate is indicated for the treatment of acute iron intoxication and of chronic iron overload due to transfusion-dependent anemias.

Acute Iron Intoxication

Deferoxamine mesylate is an adjunct to, and not a substitute for, standard measures used in treating acute iron intoxication, which may include the following: induction of emesis with syrup of ipecac; gastric lavage; suction and maintenance of a clear airway; control of shock with intravenous fluids, blood, oxygen, and vasopressors; and correction of acidosis.

Chronic Iron Overload

Deferoxamine mesylate can promote iron excretion in patients with secondary iron overload from multiple transfusions (as may occur in the treatment of some chronic anemias, including thalassemia). Long-term therapy with Deferoxamine mesylate slows accumulation of hepatic iron and retards or eliminates progression of hepatic fibrosis.

Iron mobilization with Deferoxamine mesylate is relatively poor in patients under the age of 3 years with relatively little iron overload. The drug should ordinarily not be given to such patients unless significant iron mobilization (e.g., 1 mg or more of iron per day) can be demonstrated.

Deferoxamine mesylate is not indicated for the treatment of primary hemochromatosis, since phlebotomy is the method of choice for removing excess iron in this disorder.

Contraindications

Known hypersensitivity to the active substance.

Deferoxamine mesylate is contraindicated in patients with severe renal disease or anuria, since the drug and the iron chelate are excreted primarily by the kidney. (See WARNINGS.)

Warnings

Ocular and auditory disturbances have been reported when Deferoxamine mesylate was administered over prolonged periods of time, at high doses, or in patients with low ferritin levels. The ocular disturbances observed have been blurring of vision; cataracts after prolonged administration in chronic iron overload; decreased visual acuity including visual loss, visual defects, scotoma; impaired peripheral, color, and night vision; optic neuritis, cataracts, corneal opacities, and retinal pigmentary abnormalities. The auditory abnormalities reported have been tinnitus and hearing loss including high frequency sensorineural hearing loss. In most cases, both ocular and auditory disturbances were reversible upon immediate cessation of treatment (see PRECAUTIONS/Information for patients  and ADVERSE REACTIONS/Special Senses: ).

Visual acuity tests, slit-lamp examinations, funduscopy and audiometry are recommended periodically in patients treated for prolonged periods of time. Toxicity is more likely to be reversed if symptoms or test abnormalities are detected early.

Increases in serum creatinine (possibly dose-related), acute renal failure and renal tubular disorders, associated with the administration of Deferoxamine, have been reported in postmarketing experience (see ADVERSE REACTIONS).

High doses of Deferoxamine mesylate and concomitant low ferritin levels have also been associated with growth retardation. After reduction of Deferoxamine mesylate dose, growth velocity may partially resume to pretreatment rates (see PRECAUTIONS/Pediatric use).

Adult respiratory distress syndrome, also reported in children, has been described following treatment with excessively high intravenous doses of Deferoxamine mesylate in patients with acute iron intoxication or thalassemia.

Precautions

General

Flushing of the skin, urticaria, hypotension, and shock have occurred in a few patients when Deferoxamine mesylate was administered by rapid intravenous injection. THEREFORE, Deferoxamine MESYLATE SHOULD BE GIVEN INTRAMUSCULARLY OR BY SLOW SUBCUTANEOUS OR INTRAVENOUS INFUSION.

Iron overload increases susceptibility of patients to Yersinia enterocolitica and Yersinia pseudotuberculosis infections. In some rare cases, treatment with Deferoxamine mesylate has enhanced this susceptibility, resulting in generalized infections by providing this bacteria with a siderophore otherwise missing. In such cases, Deferoxamine mesylate treatment should be discontinued until the infection is resolved.

In patients receiving Deferoxamine mesylate, rare cases of mucormycosis, some with a fatal outcome, have been reported. If any of the suspected signs or symptoms occur, Deferoxamine mesylate should be discontinued, mycological tests carried out and appropriate treatment instituted immediately.

In patients with severe chronic iron overload, impairment of cardiac function has been reported following concomitant treatment with Deferoxamine mesylate and high doses of vitamin C (more than 500 mg daily in adults). The cardiac dysfunction was reversible when vitamin C was discontinued. The following precautions should be taken when vitamin C and Deferoxamine mesylate are to be used concomitantly:

• Vitamin C supplements should not be given to patients with cardiac failure.


• Start supplemental vitamin C only after an initial month of regular treatment with Deferoxamine mesylate.


• Give vitamin C only if the patient is receiving Deferoxamine mesylate regularly, ideally soon after setting up the infusion pump.


• Do not exceed a daily vitamin C dose of 200 mg in adults, given in divided doses.


• Clinical monitoring of cardiac function is advisable during such combined therapy.

In patients with aluminum-related encephalopathy, high doses of Deferoxamine mesylate may exacerbate neurological dysfunction (seizures), probably owing to an acute increase in circulating aluminum. Deferoxamine mesylate may precipitate the onset of dialysis dementia. Treatment with Deferoxamine mesylate in the presence of aluminum overload may result in decreased serum calcium and aggravation of hyperparathyroidism.

Interactions

Drug interactions

Vitamin C:

Patients with iron overload usually become vitamin C deficient, probably because iron oxidizes the vitamin. As an adjuvant to iron chelation therapy, vitamin C in doses up to 200 mg for adults may be given in divided doses, starting after an initial month of regular treatment with Deferoxamine mesylate (see PRECAUTIONS). Vitamin C increases availability of iron for chelation. In general, 50 mg daily suffices for children under 10 years old and 100 mg daily for older children. Larger doses of vitamin C fail to produce any additional increase in excretion of iron complex.

Prochlorperazine:

Concurrent treatment with Deferoxamine mesylate and prochlorperazine, a phenothiazine derivative, may lead to temporary impairment of consciousness.

Gallium-67:

Imaging results may be distorted because of the rapid urinary excretion of Deferoxamine mesylate-bound gallium-67. Discontinuation of Deferoxamine mesylate 48 hours prior to scintigraphy is advisable.

Information for patients

Patients experiencing dizziness or other nervous system disturbances, or impairment of vision or hearing, should refrain from driving or operating potentially hazardous machines (see ADVERSE REACTIONS).

Patients should be informed that occasionally their urine may show a reddish discoloration.

Carcinogenesis, mutagenesis, impairment of fertility

Long-term carcinogenicity studies in animals have not been performed with Deferoxamine mesylate.

Cytotoxicity may occur, since Deferoxamine mesylate has been shown to inhibit DNA synthesis in vitro.

Pregnancy

Pregnancy Category C

Delayed ossification in mice and skeletal anomalies in rabbits were observed after Deferoxamine mesylate was administered in daily doses up to 4.5 times the maximum daily human dose. No adverse effects were observed in similar studies in rats.

There are no adequate and well-controlled studies in pregnant women. Deferoxamine mesylate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Deferoxamine mesylate is administered to a nursing woman.

Pediatric use

Pediatric patients receiving Deferoxamine mesylate should be monitored for body weight and growth every 3 months. Safety and effectiveness in pediatric patients under the age of 3 years have not been established (see INDICATIONS AND USAGE, WARNINGS, PRECAUTIONS/Drug interactions/ Vitamin C: , and ADVERSE REACTIONS).

Geriatric use

Clinical studies of Deferoxamine mesylate did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from the younger subjects. Postmarketing reports suggest a possible trend for an increased risk of eye disorders in the geriatric population, specifically the occurrence of color blindness, maculopathy, and scotoma. However, it is unclear if these eye disorders were dose-related. Although the number of reports was very small, certain elderly patients may be predisposed to eye disorders when taking Deferoxamine mesylate. Postmarketing reports also suggest that there may be an increased risk of deafness and hearing loss in the geriatric population. (See ADVERSE REACTIONS.) In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Adverse Reactions

The following adverse reactions have been observed, but there are not enough data to support an estimate of their frequency.

At the Injection Site:

Localized irritation, pain, burning, swelling, induration, infiltration, pruritus, erythema, wheal formation, eschar, crust, vesicles, local edema. Injection site reactions may be associated with systemic allergic reactions (see Body as a Whole: , below).

Hypersensitivity Reactions and Systemic Allergic Reactions:

Generalized rash, urticaria, anaphylactic reaction with or without shock, angioedema.

Body as a Whole: 

Local injection site reactions may be accompanied by systemic reactions like arthralgia, fever, headache, myalgia, nausea, vomiting, abdominal pain, or asthma.

Infections with Yersinia and Mucormycosis have been reported in association with Deferoxamine mesylate use (see PRECAUTIONS).

Cardiovascular:

Tachycardia, hypotension, shock.

Digestive:

Abdominal discomfort, diarrhea, nausea, vomiting.

Hematologic:

Blood dyscrasia (thrombocytopenia, leukopenia)

Musculoskeletal:

Muscle spasms. Growth retardation and bone changes (e.g., metaphyseal dysplasia) are common in chelated patients given doses above 60 mg/kg, especially those who begin iron chelation in the first three years of life. If doses are kept to 40 mg/kg or below, the risk may be reduced (see WARNINGS, PRECAUTIONS/Pediatric use).

Nervous System:

Neurological disturbances including dizziness, peripheral sensory, motor, or mixed neuropathy, paresthesias; seisures; exacerbation or precipitation of aluminum-related dialysis encephalopathy (see PRECAUTIONS/Information for patients).

Special Senses: 

High-frequency sensorineural hearing loss and/or tinnitus are uncommon if dosage guidelines are not exceeded and if dose is reduced when ferritin levels decline. Visual disturbances are rare if dosage guidelines are not exceeded. These may include decreased acuity, blurred vision, loss of vision, dyschromatopsia, night blindness, visual field defects, scotoma, retinopathy (pigmentary degeneration), optic neuritis, and cataracts (see WARNINGS).

Respiratory:

Acute respiratory distress syndrome (with dyspnea, cyanosis, and/or interstitial infiltrates) (see WARNINGS).

Skin:

Very rare generalized rash.

Urogenital:

Dysuria, acute renal failure, increased serum creatinine and renal tubular disorders (see CONTRAINDICATIONS and WARNINGS).

Postmarketing Reports

There are postmarketing reports of Deferoxamine-associated renal dysfunction, including renal failure. Monitor patients for change in renal function (e.g. increased serum creatinine).

Overdosage

Acute Toxicity

Intravenous LD50s (mg/kg): mice, 287; rats, 329.

Signs and Symptoms

Inadvertent administration of an overdose or inadvertent intravenous bolus administration/rapid intravenous infusion may be associated with hypotension, tachycardia and gastrointestinal disturbances; acute but transient loss of vision, aphasia, agitation, headache, nausea, pallor, CNS depression including coma, bradycardia and acute renal failure have been reported.

Treatment

There is no specific antidote. Deferoxamine mesylate should be discontinued and appropriate symptomatic measures undertaken.

Deferoxamine mesylate is readily dialyzable.

Deferoxamine Dosage and Administration

Acute Iron Intoxication

Intramuscular Administration

This route is preferred and should be used for ALL PATIENTS NOT IN SHOCK.

A dose of 1000 mg should be administered initially. This may be followed by 500 mg every 4 hours for two doses. Depending upon the clinical response, subsequent doses of 500 mg may be administered every 4 to 12 hours. The total amount administered should not exceed 6000 mg in 24 hours. For reconstitution instructions for intramuscular administration see Table 1 below.

 

Table 1: Preparation for Intramuscular Administration

RECONSTITUTE Deferoxamine MESYLATE WITH STERILE WATER FOR INJECTION
Vial Size	Amount of Sterile Water for Injection Required for Reconstitution	Total Drug Content after Reconstitution	Final Concentration per mL after Reconstitution
500 mg	2 mL	500 mg/2.35 mL	213 mg/mL
2 grams	8 mL	2 grams/9.4 mL	213 mg/mL

The reconstituted Deferoxamine mesylate solution is a yellow-colored solution. The drug should be completely dissolved before the solution is withdrawn. Deferoxamine mesylate reconstituted with Sterile Water for Injection IS FOR SINGLE USE ONLY. Discard unused portion.

Intravenous Administration

THIS ROUTE SHOULD BE USED ONLY FOR PATIENTS IN A STATE OF CARDIOVASCULAR COLLAPSE AND THEN ONLY BY SLOW INFUSION. THE RATE OF INFUSION SHOULD NOT EXCEED 15 MG/KG/HR FOR THE FIRST 1000 MG ADMINISTERED. SUBSEQUENT IV DOSING, IF NEEDED, MUST BE AT A SLOWER RATE, NOT TO EXCEED 125 MG/HR.

The reconstituted solution is added to physiologic saline (e.g., 0.9% sodium chloride, 0.45% sodium chloride), glucose in water, or Ringer's lactate solution.

An initial dose of 1000 mg should be administered at a rate NOT TO EXCEED 15 mg/kg/hr. This may be followed by 500 mg over 4 hours for two doses. Depending upon the clinical response, subsequent doses of 500 mg may be administered over 4 to 12 hours. The total amount administered should not exceed 6000 mg in 24 hours.

As soon as the clinical condition of the patient permits, intravenous administration should be discontinued and the drug should be administered intramuscularly. For reconstitution instructions for intravenous administration see Table 2 below.

Table 2: Preparation for Intravenous Administration

RECONSTITUTE Deferoxamine MESYLATE WITH STERILE WATER FOR INJECTION
Vial Size	Amount of Sterile Water for Injection Required for Reconstitution	Total Drug Content after Reconstitution	Final Concentration per mL after Reconstitution
500 mg	5 mL	500 mg/5.3 mL	95 mg/mL
2 grams	20 mL	2 grams/21.1 mL	95 mg/mL

 

The reconstituted Deferoxamine mesylate solution is an isotonic, clear and colorless to slightly yellowish solution. The drug should be completely dissolved before the solution is withdrawn. Deferoxamine mesylate reconstituted with Sterile Water for Injection IS FOR SINGLE USE ONLY. Discard unused portion.

Chronic Iron Overload

The more effective of the following routes of administration must be chosen on an individual basis for each patient.

Intramuscular Administration

A daily dose of 500 to 1000 mg should be administered intramuscularly. In addition, 2000 mg should be administered intravenously with each unit of blood transfused; however, Deferoxamine mesylate should be administered separately from the blood. The rate of intravenous infusion must not exceed 15 mg/kg/hr. The total daily dose should not exceed 1000 mg in the absence of a transfusion, or 6000 mg even if transfused three or more units of blood or packed red blood cells. For reconstitution instructions for intramuscular administration see Table 3 below.

Table 3: Preparation for Intramuscular Administration

RECONSTITUTE Deferoxamine MESYLATE WITH STERILE WATER FOR INJECTION
Vial Size	Amount of Sterile Water for Injection Required for Reconstitution	Total Drug Content after Reconstitution	Final Concentration per mL after Reconstitution
500 mg	2 mL	500 mg/2.35 mL	213 mg/mL
2 grams	8 mL	2 grams/9.4 mL	213 mg/mL

 

The reconstituted Deferoxamine mesylate solution is a yellow-colored solution. The drug should be completely dissolved before the solution is withdrawn. Deferoxamine mesylate reconstituted with Sterile Water for Injection IS FOR SINGLE USE ONLY. Discard unused portion.

Subcutaneous Administration

A daily dose of 1000 to 2000 mg (20 to 40 mg/kg/day) should be administered over 8 to 24 hours, utilizing a small portable pump capable of providing continuous mini-infusion. The duration of infusion must be individualized. In some patients, as much iron will be excreted after a short infusion of 8 to 12 hours as with the same dose given over 24 hours. For reconstitution instructions for subcutaneous administration see Table 4 below.

Table 4: Preparation for Subcutaneous Administration

RECONSTITUTE Deferoxamine MESYLATE WITH STERILE WATER FOR INJECTION
Vial Size	Amount of Sterile Water for Injection Required for Reconstitution	Total Drug Content after Reconstitution	Final Concentration per mL after Reconstitution
500 mg	5 mL	500 mg/5.3 mL	95 mg/mL
2 grams	20 mL	2 grams/21.1 mL	95 mg/mL

The reconstituted Deferoxamine mesylate solution is an isotonic, clear and colorless to slightly-yellowish solution. The drug should be completely dissolved before the solution is withdrawn. Deferoxamine mesylate reconstituted with Sterile Water for Injection IS FOR SINGLE USE ONLY. Discard unused portion.

Stability after Reconstitution

The product should be used immediately after reconstitution (commencement of treatment within 3 hours) for microbiological safety. When reconstitution is carried out under validated aseptic conditions (in a sterile laminar flow hood using aseptic technique), the product may be stored at room temperature for a maximum period of 24 hours before use. Do not refrigerate reconstituted solution. Reconstituting Deferoxamine mesylate in solvents or under conditions other than indicated may result in precipitation. Turbid solutions should not be used.

How is Deferoxamine Supplied

Deferoxamine Mesylate for Injection USP in single dose vials, each containing 500 mg and 2 g of sterile, lyophilized Deferoxamine mesylate, is available as follows:

NDC 55390-263-10; 500 mg per vial, carton of 10.

NDC 55390-265-01; 2 g per vial, individually boxed.

Each vial is for single use only. Discard unused portion of the solution.

Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.]

Manufactured by:	Manufactured for:
Ben Venue Laboratories, Inc.	Bedford Laboratories™
Bedford, OH 44146	Bedford, OH 44146
October 2010	DEF-P02

VIAL LABEL 500 MG

Vial Label 500 mg

VIAL LABEL 2 GRAM

Vial Label 2 Grams

Deferoxamine MESYLATE  Deferoxamine mesylate  injection, powder, lyophilized, for solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 55390-263 Route of Administration INTRAMUSCULAR, INTRAVENOUS, SUBCUTANEOUS DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength Deferoxamine MESYLATE (Deferoxamine) Deferoxamine MESYLATE 500 mg  in 5.3 mL

Inactive Ingredients Ingredient Name Strength No Inactive Ingredients Found

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 55390-263-10 10 VIAL In 1 BOX contains a VIAL 1 10 mL In 1 VIAL This package is contained within the BOX (55390-263-10)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA078086	06/18/2010

Deferoxamine MESYLATE  Deferoxamine mesylate  injection, powder, lyophilized, for solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 55390-265 Route of Administration INTRAMUSCULAR, INTRAVENOUS, SUBCUTANEOUS DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength Deferoxamine MESYLATE (Deferoxamine) Deferoxamine MESYLATE 2 g  in 21.1 mL

Inactive Ingredients Ingredient Name Strength No Inactive Ingredients Found

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 55390-265-01 1 VIAL In 1 BOX contains a VIAL 1 20 mL In 1 VIAL This package is contained within the BOX (55390-265-01)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA078086	06/18/2010

Labeler - Bedford Laboratories (884528407)

Establishment
Name	Address	ID/FEI	Operations
Ben Venue Laboratories		004327953	MANUFACTURE

Revised: 06/2011Bedford Laboratories

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